SELGANTOLIMOD

SELGANTOLIMOD : Agonist of TLR8

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe SELGANTOLIMOD is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

TLR8

Agonist

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q9NR97

Target Class: GPCR

Target SubClass: Toll-like receptor

PDB ID for probe-target interaction (3D structure): 6WML

Target aliases:

Toll-like receptor 8, TLR8, TLR8_HUMAN

DOI Reference: 10.1021/acs.jmedchem.0c00100

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): The broader selectivity profile of (R)-7 toward immune receptors was assessed in reporter gene assays using HEK293 cells, stably expressing individual human TLRs or other innate immune receptors. Moreover, (R)-7 did not stimulate HEK293 cells stably expressing other human TLRs including TLR2, TLR3, TLR4, TLR5, TLR9, and other receptors including Nod-like receptors (NLRs: NOD1 and NOD2), RIG-I -like receptors (RLRs; RIG-I and MDA5), or C-type lectin receptors (CLRs; Dectin1a, Dectin 1b, and Mincle).

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Although there is no direct demonstration of in-cell target engagement and PD biomarkers are quite distal (cytokine and reporter gene endpoints), the lack of activity across a range of related receptors and the structural data supporting the SAR point to a potent and selective TLR8 agonist.

(last updated: 18 Oct 2022 )

SERP Ratings

In Model Organisms

SERP Comments:

Extensive validation supports (R)-7 as a probe with excellent selectivity for TRL8 among the TRL family. Although biophysical characterization is limited, this probe has been well characterized in cells and model organisms for its intended use.

(last updated: 20 Oct 2022 )